JP2016518434A5 - - Google Patents

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JP2016518434A5
JP2016518434A5 JP2016513385A JP2016513385A JP2016518434A5 JP 2016518434 A5 JP2016518434 A5 JP 2016518434A5 JP 2016513385 A JP2016513385 A JP 2016513385A JP 2016513385 A JP2016513385 A JP 2016513385A JP 2016518434 A5 JP2016518434 A5 JP 2016518434A5
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本発明は、以下の態様を包含し得る。  The present invention may include the following aspects.
［１］[1]
式（ＩＤ）  Formula (ID)


［式中：[Where:
各Ｘは独立してＣＲ  Each X is independently CR ７7 を表し、Represents
Ｒ  R ａa 、Ｒ, R ｂb およびＲAnd R ｃc は、水素、フルオロ、ブロモ、クロロ、−ＣＨＦIs hydrogen, fluoro, bromo, chloro, -CHF ２2 、−ＣＦ, -CF ２2 −メチル、−ＣＨ-Methyl, -CH ２2 Ｆ、−ＣＦF, -CF ３3 、−ＯＣＦ, -OCF ３3 、−ＣＮ、Ｃ, -CN, C １1 〜Ｃ~ C ３3 アルキルおよびＣAlkyl and C ３3 〜Ｃ~ C ４4 シクロアルキルからなる群から独立して選択され、Independently selected from the group consisting of cycloalkyl;
Ｒ  R ｄd は水素またはフルオロであり、Is hydrogen or fluoro;
Ｒ  R ４4 は、水素、ＣIs hydrogen, C １1 〜Ｃ~ C ３3 アルキルまたはＣAlkyl or C ３3 〜Ｃ~ C ４4 シクロアルキルであり、Cycloalkyl,
Ｒ  R ５5 は水素であり、Is hydrogen,
Ｒ  R ６6 は、ＣIs C ２2 〜Ｃ~ C ６6 アルキル、１個以上のフルオロで任意選択により置換されているＣAlkyl, C optionally substituted with one or more fluoro １1 〜Ｃ~ C ４4 アルキル−ＲAlkyl-R ８8 、１個以上のフルオロで任意選択により置換されているＣC optionally substituted with one or more fluoro １1 〜Ｃ~ C ４4 アルキル−ＲAlkyl-R ９9 、ならびにＯ、ＳおよびＮからなる群からそれぞれ独立して選択される１個以上のヘテロ原子を任意選択により含有する３〜７員の単環式または多環式飽和環からなる群から選択され、このような３〜７員飽和環またはＣSelected from the group consisting of 3-7 membered monocyclic or polycyclic saturated rings optionally containing one or more heteroatoms independently selected from the group consisting of O, S and N Such a 3-7 membered saturated ring or C ２2 〜Ｃ~ C ６6 アルキルは、水素、−ＯＨ、フルオロ、オキソ、ＲAlkyl is hydrogen, —OH, fluoro, oxo, R ９9 、Ｒ, R １０10 、およびＲAnd R １０10 で任意選択により置換されているＣOptionally substituted with C １1 〜Ｃ~ C ４4 アルキルからなる群からそれぞれ独立して選択される１個以上の置換基で、任意選択により置換されており、Optionally substituted with one or more substituents each independently selected from the group consisting of alkyl,
Ｒ  R ７7 は、水素、−ＣＮ、フルオロ、クロロ、ブロモ、−ＣＨＦIs hydrogen, -CN, fluoro, chloro, bromo, -CHF ２2 、−ＣＦ, -CF ２2 −メチル、−ＣＨ-Methyl, -CH ２2 Ｆ、−ＣＦF, -CF ３3 、メトキシで任意選択により置換されているＣC optionally substituted with methoxy １1 〜Ｃ~ C ３3 アルキル、ＣAlkyl, C ２2 〜Ｃ~ C ３3 アルケニルまたはＣAlkenyl or C ３3 〜Ｃ~ C ４4 シクロアルキルを表し、Represents cycloalkyl,
Ｒ  R ８8 は、Ｏ、ＳおよびＮからなる群からそれぞれ独立して選択される１個以上のヘテロ原子を任意選択により含有する３〜７員飽和環を表し、このような３〜７員飽和環は、ＲRepresents a 3-7 membered saturated ring optionally containing one or more heteroatoms, each independently selected from the group consisting of O, S and N, such 3-7 membered saturated ring, R １０10 で任意選択により置換されている１個以上のＣOne or more C optionally substituted with １1 〜Ｃ~ C ４4 アルキルで、任意選択により置換されており、Optionally substituted with alkyl;
Ｒ  R ９9 は、ＣIs C １1 〜Ｃ~ C ４4 アルキルオキシ、−ＳＯAlkyloxy, -SO ２2 −メチル、−Ｃ（＝Ｏ）−ＯＲ-Methyl, -C (= O) -OR １１11 または−Ｃ（＝Ｏ）−Ｎ（ＲOr -C (= O) -N (R １１11 ）) ２2 を表し、Represents
Ｒ  R １０10 は、−ＣＮ、−ＯＨ、フルオロ、−ＣＨＦIs —CN, —OH, fluoro, —CHF ２2 、−ＣＨ, -CH ２2 Ｆまたは−ＣＦF or -CF ３3 を表し、Represents
Ｒ  R １１11 は水素またはＣIs hydrogen or C １1 〜Ｃ~ C ３3 アルキルを表す］Represents alkyl]
の化合物であって、このような化合物が、Wherein such a compound is


でもない化合物、もしくはその立体異性体もしくは互変異性体、またはその薬学的に許容される塩もしくは溶媒和物。Or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt or solvate thereof.
［２］[2]
式（ＩＢ）  Formula (IB)


を有する上記［１］に記載の化合物。[1] The compound according to [1] above.
［３］[3]
Ｒ  R ４4 がメチルである、上記［１］または［２］に記載の化合物。The compound according to [1] or [2] above, wherein is methyl.
［４］[4]
Ｒ  R ６6 が、１個の酸素を任意選択により含有する３〜７員飽和環を含有する、上記［１］〜［３］のいずれか一項に記載の化合物。The compound according to any one of [1] to [3] above, which contains a 3 to 7 membered saturated ring optionally containing one oxygen.
［５］[5]
Ｒ  R ６6 が、１個の酸素を含有する４員または５員飽和環であり、このような４員または５員飽和環が、ＲIs a 4- or 5-membered saturated ring containing one oxygen and such 4- or 5-membered saturated ring is R １０10 で任意選択により置換されているＣOptionally substituted with C １1 〜Ｃ~ C ４4 アルキルで任意選択により置換されている、上記［１］〜［４］のいずれか一項に記載の化合物。The compound according to any one of [1] to [4] above, which is optionally substituted with alkyl.
［６］[6]
Ｒ  R ６6 が、１個以上のフルオロで任意選択により置換されている分岐鎖ＣA branched chain C is optionally substituted with one or more fluoro ３3 〜Ｃ~ C ６6 アルキルを含むか、あるいはＲContains alkyl or R ６6 がＣIs C ３3 〜Ｃ~ C ６6 シクロアルキルを含み、このようなＣIncluding cycloalkyl, such C ３3 〜Ｃ~ C ６6 シクロアルキルは１個以上のフルオロで置換されている、または１個以上のフルオロで置換されたＣCycloalkyl is C substituted with one or more fluoro, or substituted with one or more fluoro １1 〜Ｃ~ C ４4 アルキルで置換されているか、あるいはＲSubstituted with alkyl or R ６6 がＣIs C ３3 〜Ｃ~ C ６6 シクロアルキルを含み、このようなＣIncluding cycloalkyl, such C ３3 〜Ｃ~ C ６6 シクロアルキルは、１個以上のフルオロで任意選択により置換されている、および／または１個以上のフルオロで任意選択により置換されたＣCycloalkyl is C optionally substituted with one or more fluoro and / or optionally substituted with one or more fluoro. １1 〜Ｃ~ C ４4 アルキルで置換されている、上記［１］〜［３］のいずれか一項に記載の化合物。The compound according to any one of [1] to [3], which is substituted with alkyl.
［７］[7]
Ｒ  R ６6 が、１個以上のフルオロで置換されている分岐鎖ＣIs a branched chain C substituted with one or more fluoro ３3 〜Ｃ~ C ６6 アルキルである、上記［６］に記載の化合物。The compound according to [6] above, which is alkyl.
［８］[8]
Ｒ  R ｂb が水素またはフルオロである、上記［１］〜［７］のいずれか一項に記載の化合物。The compound according to any one of [1] to [7] above, wherein is hydrogen or fluoro.
［９］[9]
Ｒ  R ａa およびＲAnd R ｃc が、水素、フルオロ、クロロ、ＣＮおよびメチルからなる群から独立して選択される、上記［１］〜［８］のいずれか一項に記載の化合物。The compound according to any one of [1] to [8] above, wherein is independently selected from the group consisting of hydrogen, fluoro, chloro, CN and methyl.
［１０］[10]
式（ＩＣ）  Formula (IC)


［式中：[Where:
ＸはＣＲ  X is CR ７7 を表し、Represents
Ｒ  R ａa 、Ｒ, R ｂb およびＲAnd R ｃc は、水素、フルオロ、ブロモ、クロロ、−ＣＨＦIs hydrogen, fluoro, bromo, chloro, -CHF ２2 、−ＣＦ, -CF ２2 −メチル、−ＣＨ-Methyl, -CH ２2 Ｆ、−ＣＦF, -CF ３3 、−ＯＣＦ, -OCF ３3 、−ＣＮ、Ｃ, -CN, C １1 〜Ｃ~ C ３3 アルキルおよびＣAlkyl and C ３3 〜Ｃ~ C ４4 シクロアルキルからなる群から独立して選択され、Independently selected from the group consisting of cycloalkyl;
Ｒ  R ４4 は、水素、ＣIs hydrogen, C １1 〜Ｃ~ C ３3 アルキルまたはＣAlkyl or C ３3 〜Ｃ~ C ４4 シクロアルキルであり、Cycloalkyl,
Ｒ  R ５5 は水素であり、Is hydrogen,
Ｒ  R ６6 は、ＣIs C ２2 〜Ｃ~ C ６6 アルキル、１個以上のフルオロで任意選択により置換されているＣAlkyl, C optionally substituted with one or more fluoro １1 〜Ｃ~ C ４4 アルキル−ＲAlkyl-R ８8 、１個以上のフルオロで任意選択により置換されているＣC optionally substituted with one or more fluoro １1 〜Ｃ~ C ４4 アルキル−ＲAlkyl-R ９9 、ならびにＯ、ＳおよびＮからなる群からそれぞれ独立して選択される１個以上のヘテロ原子を任意選択により含有する３〜７員の単環式または多環式飽和環からなる群から選択され、このような３〜７員飽和環またはＣSelected from the group consisting of 3-7 membered monocyclic or polycyclic saturated rings optionally containing one or more heteroatoms independently selected from the group consisting of O, S and N Such a 3-7 membered saturated ring or C ２2 〜Ｃ~ C ６6 アルキルは、水素、−ＯＨ、フルオロ、オキソ、ＲAlkyl is hydrogen, —OH, fluoro, oxo, R ９9 、Ｒ, R １０10 、およびＲAnd R １０10 で任意選択により置換されているＣOptionally substituted with C １1 〜Ｃ~ C ４4 アルキルからなる群からそれぞれ独立して選択される１個以上の置換基で、任意選択により置換されており、Optionally substituted with one or more substituents each independently selected from the group consisting of alkyl,
Ｒ  R ７7 は、水素、−ＣＮ、フルオロ、クロロ、ブロモ、−ＣＨＦIs hydrogen, -CN, fluoro, chloro, bromo, -CHF ２2 、−ＣＦ, -CF ２2 −メチル、−ＣＨ-Methyl, -CH ２2 Ｆ、−ＣＦF, -CF ３3 、Ｃ, C １1 〜Ｃ~ C ３3 アルキルまたはＣAlkyl or C ３3 〜Ｃ~ C ４4 シクロアルキルを表し、Represents cycloalkyl,
Ｒ  R ８8 は、Ｏ、ＳおよびＮからなる群からそれぞれ独立して選択される１個以上のヘテロ原子を任意選択により含有する３〜７員飽和環を表し、このような３〜７員飽和環は、ＲRepresents a 3-7 membered saturated ring optionally containing one or more heteroatoms, each independently selected from the group consisting of O, S and N, such 3-7 membered saturated ring, R １０10 で任意選択により置換されている１個以上のＣOne or more C optionally substituted with １1 〜Ｃ~ C ４4 アルキルで、任意選択により置換されており、Optionally substituted with alkyl;
Ｒ  R ９9 は、ＣIs C １1 〜Ｃ~ C ４4 アルキルオキシ、−ＳＯAlkyloxy, -SO ２2 −メチル、−Ｃ（＝Ｏ）−ＯＲ-Methyl, -C (= O) -OR １１11 または−Ｃ（＝Ｏ）−Ｎ（ＲOr -C (= O) -N (R １１11 ）) ２2 を表し、Represents
Ｒ  R １０10 は、−ＣＮ、−ＯＨ、フルオロ、−ＣＨＦIs —CN, —OH, fluoro, —CHF ２2 、−ＣＨ, -CH ２2 Ｆまたは−ＣＦF or -CF ３3 を表し、Represents
Ｒ  R １１11 は水素またはＣIs hydrogen or C １1 〜Ｃ~ C ３3 アルキルを表す］Represents alkyl]
を有する、上記［１］〜［９］のいずれか一項に記載の化合物であって、このような化合物が、The compound according to any one of [1] to [9] above, wherein such a compound is


でもない化合物、もしくはその立体異性体もしくは互変異性体、またはその薬学的に許容される塩もしくは溶媒和物。Or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt or solvate thereof.
［１１］[11]
Ｒ  R ４4 がＣIs C １1 〜Ｃ~ C ３3 アルキルであり、Alkyl,
Ｒ  R ６6 が、１個以上のフルオロで任意選択により置換されているＣIs optionally substituted with one or more fluoro ２2 〜Ｃ~ C ６6 アルキルからなる群から選択され、Selected from the group consisting of alkyl,
Ｒ  R ７7 が、水素、フルオロ、クロロまたはＣIs hydrogen, fluoro, chloro or C １1 〜Ｃ~ C ３3 アルキルを表す、Represents alkyl,
上記［１０］に記載の化合物。The compound according to the above [10].
［１２］[12]
Ｒ  R ４4 がメチルを表し、ＲRepresents methyl and R ６6 が、１個以上のフルオロで置換されているＣC substituted with one or more fluoro ２2 〜Ｃ~ C ６6 アルキルであり、ＲAlkyl and R ７7 が水素を表し、ＲRepresents hydrogen and R ａa 、Ｒ, R ｂb およびＲAnd R ｃc が、水素、フルオロ、クロロ、メチルおよび−ＣＮからなる群から独立して選択される、上記［１］〜［１１］のいずれか一項に記載の化合物。The compound according to any one of [1] to [11], wherein is independently selected from the group consisting of hydrogen, fluoro, chloro, methyl, and -CN.
［１３］[13]
哺乳動物におけるＨＢＶ感染の予防または処置に使用される、上記［１］〜［１２］のいずれか一項に記載の化合物。  The compound according to any one of [1] to [12] above, which is used for prevention or treatment of HBV infection in a mammal.
［１４］[14]
上記［１］〜［１３］のいずれか一項に記載の化合物と、薬学的に許容される担体とを含む医薬組成物。  A pharmaceutical composition comprising the compound according to any one of [1] to [13] above and a pharmaceutically acceptable carrier.
［１５］[15]
ＨＢＶ感染の処置において同時に、別々に、または順次使用される併用剤として、（ａ）上記［１］〜［１３］のいずれか一項に記載の式（ＩＤ）の化合物と、（ｂ）別のＨＢＶ阻害剤とを含有する製品。  As a concomitant agent used simultaneously, separately or sequentially in the treatment of HBV infection, (a) the compound of formula (ID) according to any one of [1] to [13] above, and (b) A product containing a HBV inhibitor.

Claims (37)

式（ＩＤ）


［式中：
各Ｘは独立してＣＲ７を表し、
Ｒａ、ＲｂおよびＲｃは、水素、フルオロ、ブロモ、クロロ、−ＣＨＦ２、−ＣＦ２−メチル、−ＣＨ２Ｆ、−ＣＦ３、−ＯＣＦ３、−ＣＮ、Ｃ１〜Ｃ３アルキルおよびＣ３〜Ｃ４シクロアルキルからなる群から独立して選択され、
Ｒｄは水素またはフルオロであり、
Ｒ４は、水素、Ｃ１〜Ｃ３アルキルまたはＣ３〜Ｃ４シクロアルキルであり、
Ｒ５は水素であり、
Ｒ６は、Ｃ２〜Ｃ６アルキル、１個以上のフルオロで任意選択により置換されているＣ１〜Ｃ４アルキル−Ｒ８、１個以上のフルオロで任意選択により置換されているＣ１〜Ｃ４アルキル−Ｒ９、ならびにＯ、ＳおよびＮからなる群からそれぞれ独立して選択される１個以上のヘテロ原子を任意選択により含有する３〜７員の単環式または多環式飽和環からなる群から選択され、このような３〜７員飽和環またはＣ２〜Ｃ６アルキルは、水素、−ＯＨ、フルオロ、オキソ、Ｒ９、Ｒ１０、およびＲ１０で任意選択により置換されているＣ１〜Ｃ４アルキルからなる群からそれぞれ独立して選択される１個以上の置換基で、任意選択により置換されており、
Ｒ７は、水素、−ＣＮ、フルオロ、クロロ、ブロモ、−ＣＨＦ２、−ＣＦ２−メチル、−ＣＨ２Ｆ、−ＣＦ３、メトキシで任意選択により置換されているＣ１〜Ｃ３アルキル、Ｃ２〜Ｃ３アルケニルまたはＣ３〜Ｃ４シクロアルキルを表し、
Ｒ８は、Ｏ、ＳおよびＮからなる群からそれぞれ独立して選択される１個以上のヘテロ原子を任意選択により含有する３〜７員飽和環を表し、このような３〜７員飽和環は、Ｒ１０で任意選択により置換されている１個以上のＣ１〜Ｃ４アルキルで、任意選択により置換されており、
Ｒ９は、Ｃ１〜Ｃ４アルキルオキシ、−ＳＯ２−メチル、−Ｃ（＝Ｏ）−ＯＲ１１または−Ｃ（＝Ｏ）−Ｎ（Ｒ１１）２を表し、
Ｒ１０は、−ＣＮ、−ＯＨ、フルオロ、−ＣＨＦ２、−ＣＨ２Ｆまたは−ＣＦ３を表し、
Ｒ１１は水素またはＣ１〜Ｃ３アルキルを表す］
の化合物であって、このような化合物が、


でもない化合物、もしくはその立体異性体もしくは互変異性体、またはその薬学的に許容される塩もしくは溶媒和物。 Formula (ID)


[Where:
Each X independently represents CR 7 ,
R a , R b and R c are hydrogen, fluoro, bromo, chloro, —CHF 2 , —CF 2 -methyl, —CH 2 F, —CF 3 , —OCF 3 , —CN, C 1 to C 3 alkyl. And independently selected from the group consisting of C 3 -C 4 cycloalkyl,
R d is hydrogen or fluoro;
R 4 is hydrogen, C 1 -C 3 alkyl or C 3 -C 4 cycloalkyl,
R 5 is hydrogen;
R 6 is, C 2 -C 6 alkyl, C 1 are optionally substituted with C 1 -C 4 alkyl -R 8, one or more fluoro being optionally substituted with one or more fluoro ~ A 3-7 membered monocyclic or polycyclic saturated ring optionally containing one or more heteroatoms independently selected from the group consisting of C 4 alkyl-R 9 and O, S and N Such a 3-7 membered saturated ring or C 2 -C 6 alkyl is optionally substituted with hydrogen, —OH, fluoro, oxo, R 9 , R 10 , and R 10. Optionally substituted with one or more substituents each independently selected from the group consisting of C 1 -C 4 alkyl,
R 7 is C 1 -C 3 alkyl optionally substituted with hydrogen, —CN, fluoro, chloro, bromo, —CHF 2 , —CF 2 -methyl, —CH 2 F, —CF 3 , methoxy, C 2 -C 3 alkenyl or C 3 -C 4 cycloalkyl,
R 8 represents a 3-7 membered saturated ring optionally containing one or more heteroatoms independently selected from the group consisting of O, S and N, such a 3-7 membered saturated ring Is optionally substituted with one or more C 1 -C 4 alkyl optionally substituted with R 10 ;
R 9 represents C 1 -C 4 alkyloxy, —SO 2 -methyl, —C (═O) —OR 11 or —C (═O) —N (R 11 ) 2 ,
R 10 represents —CN, —OH, fluoro, —CHF 2 , —CH 2 F or —CF 3 ,
R 11 represents hydrogen or C 1 -C 3 alkyl]
Wherein such a compound is


Or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt or solvate thereof. 式（ＩＢ）


を有する請求項１に記載の化合物。 Formula (IB)


The compound of claim 1 having Ｒ４がメチルである、請求項１または２に記載の化合物。 The compound according to claim 1 or 2, wherein R 4 is methyl. Ｒ６が、１個の酸素を任意選択により含有する３〜７員飽和環を含有する、請求項１〜３のいずれか一項に記載の化合物。 R 6 is, contain 3-7 membered saturated ring containing optionally one oxygen, a compound according to any one of claims 1 to 3. Ｒ６が、１個の酸素を含有する４員または５員飽和環であり、このような４員または５員飽和環が、Ｒ１０で任意選択により置換されているＣ１〜Ｃ４アルキルで任意選択により置換されている、請求項１〜４のいずれか一項に記載の化合物。 R 6 is a 4-membered or 5-membered saturated ring containing one oxygen, and such 4-membered or 5-membered saturated ring is C 1 -C 4 alkyl optionally substituted with R 10 5. A compound according to any one of claims 1 to 4, optionally substituted. Ｒ６が、１個以上のフルオロで任意選択により置換されている分岐鎖Ｃ３〜Ｃ６アルキルを含むか、あるいはＲ６がＣ３〜Ｃ６シクロアルキルを含み、このようなＣ３〜Ｃ６シクロアルキルは１個以上のフルオロで置換されている、または１個以上のフルオロで置換されたＣ１〜Ｃ４アルキルで置換されているか、あるいはＲ６がＣ３〜Ｃ６シクロアルキルを含み、このようなＣ３〜Ｃ６シクロアルキルは、１個以上のフルオロで任意選択により置換されている、および／または１個以上のフルオロで任意選択により置換されたＣ１〜Ｃ４アルキルで置換されている、請求項１〜３のいずれか一項に記載の化合物。 R 6 contains a branched C 3 -C 6 alkyl optionally substituted with one or more fluoro, or R 6 contains a C 3 -C 6 cycloalkyl, such C 3 -C 6 6 cycloalkyl is substituted with one or more fluoro, or is substituted with C 1 -C 4 alkyl substituted with one or more fluoro, or R 6 includes C 3 -C 6 cycloalkyl such C 3 -C 6 cycloalkyl, substituted with the one or more are optionally substituted with fluoro, and / or C 1 -C 4 alkyl optionally substituted with one or more fluoro The compound according to any one of claims 1 to 3, wherein Ｒ６が、１個以上のフルオロで置換されている分岐鎖Ｃ３〜Ｃ６アルキルである、請求項６に記載の化合物。 R 6 is a branched C 3 -C 6 alkyl substituted with one or more fluoro, a compound according to claim 6. Ｒｂが水素またはフルオロである、請求項１〜７のいずれか一項に記載の化合物。 The compound according to any one of claims 1 to 7, wherein R b is hydrogen or fluoro. ＲａおよびＲｃが、水素、フルオロ、クロロ、ＣＮおよびメチルからなる群から独立して選択される、請求項１〜８のいずれか一項に記載の化合物。 9. A compound according to any one of claims 1 to 8, wherein R <a> and R <c> are independently selected from the group consisting of hydrogen, fluoro, chloro, CN and methyl. 式（ＩＣ）


［式中：
ＸはＣＲ７を表し、
Ｒａ、ＲｂおよびＲｃは、水素、フルオロ、ブロモ、クロロ、−ＣＨＦ２、−ＣＦ２−メチル、−ＣＨ２Ｆ、−ＣＦ３、−ＯＣＦ３、−ＣＮ、Ｃ１〜Ｃ３アルキルおよびＣ３〜Ｃ４シクロアルキルからなる群から独立して選択され、
Ｒ４は、水素、Ｃ１〜Ｃ３アルキルまたはＣ３〜Ｃ４シクロアルキルであり、
Ｒ５は水素であり、
Ｒ６は、Ｃ２〜Ｃ６アルキル、１個以上のフルオロで任意選択により置換されているＣ１〜Ｃ４アルキル−Ｒ８、１個以上のフルオロで任意選択により置換されているＣ１〜Ｃ４アルキル−Ｒ９、ならびにＯ、ＳおよびＮからなる群からそれぞれ独立して選択される１個以上のヘテロ原子を任意選択により含有する３〜７員の単環式または多環式飽和環からなる群から選択され、このような３〜７員飽和環またはＣ２〜Ｃ６アルキルは、水素、−ＯＨ、フルオロ、オキソ、Ｒ９、Ｒ１０、およびＲ１０で任意選択により置換されているＣ１〜Ｃ４アルキルからなる群からそれぞれ独立して選択される１個以上の置換基で、任意選択により置換されており、
Ｒ７は、水素、−ＣＮ、フルオロ、クロロ、ブロモ、−ＣＨＦ２、−ＣＦ２−メチル、−ＣＨ２Ｆ、−ＣＦ３、Ｃ１〜Ｃ３アルキルまたはＣ３〜Ｃ４シクロアルキルを表し、
Ｒ８は、Ｏ、ＳおよびＮからなる群からそれぞれ独立して選択される１個以上のヘテロ原子を任意選択により含有する３〜７員飽和環を表し、このような３〜７員飽和環は、Ｒ１０で任意選択により置換されている１個以上のＣ１〜Ｃ４アルキルで、任意選択により置換されており、
Ｒ９は、Ｃ１〜Ｃ４アルキルオキシ、−ＳＯ２−メチル、−Ｃ（＝Ｏ）−ＯＲ１１または−Ｃ（＝Ｏ）−Ｎ（Ｒ１１）２を表し、
Ｒ１０は、−ＣＮ、−ＯＨ、フルオロ、−ＣＨＦ２、−ＣＨ２Ｆまたは−ＣＦ３を表し、
Ｒ１１は水素またはＣ１〜Ｃ３アルキルを表す］
を有する、請求項１〜９のいずれか一項に記載の化合物であって、このような化合物が、


でもない化合物、もしくはその立体異性体もしくは互変異性体、またはその薬学的に許容される塩もしくは溶媒和物。 Formula (IC)


[Where:
X represents CR 7 ,
R a , R b and R c are hydrogen, fluoro, bromo, chloro, —CHF 2 , —CF 2 -methyl, —CH 2 F, —CF 3 , —OCF 3 , —CN, C 1 to C 3 alkyl. And independently selected from the group consisting of C 3 -C 4 cycloalkyl,
R 4 is hydrogen, C 1 -C 3 alkyl or C 3 -C 4 cycloalkyl,
R 5 is hydrogen;
R 6 is, C 2 -C 6 alkyl, C 1 are optionally substituted with C 1 -C 4 alkyl -R 8, one or more fluoro being optionally substituted with one or more fluoro ~ A 3-7 membered monocyclic or polycyclic saturated ring optionally containing one or more heteroatoms independently selected from the group consisting of C 4 alkyl-R 9 and O, S and N Such a 3-7 membered saturated ring or C 2 -C 6 alkyl is optionally substituted with hydrogen, —OH, fluoro, oxo, R 9 , R 10 , and R 10. Optionally substituted with one or more substituents each independently selected from the group consisting of C 1 -C 4 alkyl,
R 7 represents hydrogen, —CN, fluoro, chloro, bromo, —CHF 2 , —CF 2 -methyl, —CH 2 F, —CF 3 , C 1 -C 3 alkyl or C 3 -C 4 cycloalkyl. ,
R 8 represents a 3-7 membered saturated ring optionally containing one or more heteroatoms independently selected from the group consisting of O, S and N, such a 3-7 membered saturated ring Is optionally substituted with one or more C 1 -C 4 alkyl optionally substituted with R 10 ;
R 9 represents C 1 -C 4 alkyloxy, —SO 2 -methyl, —C (═O) —OR 11 or —C (═O) —N (R 11 ) 2 ,
R 10 represents —CN, —OH, fluoro, —CHF 2 , —CH 2 F or —CF 3 ,
R 11 represents hydrogen or C 1 -C 3 alkyl]
10. A compound according to any one of claims 1 to 9, wherein such a compound is


Or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt or solvate thereof. Ｒ４がＣ１〜Ｃ３アルキルであり、
Ｒ６が、１個以上のフルオロで任意選択により置換されているＣ２〜Ｃ６アルキルからなる群から選択され、
Ｒ７が、水素、フルオロ、クロロまたはＣ１〜Ｃ３アルキルを表す、
請求項１０に記載の化合物。 R 4 is C 1 -C 3 alkyl;
R 6 is selected from the group consisting of C 2 -C 6 alkyl optionally substituted with one or more fluoro;
R 7 represents hydrogen, fluoro, chloro or C 1 -C 3 alkyl,
11. A compound according to claim 10. Ｒ４がメチルを表し、Ｒ６が、１個以上のフルオロで置換されているＣ２〜Ｃ６アルキルであり、Ｒ７が水素を表し、Ｒａ、ＲｂおよびＲｃが、水素、フルオロ、クロロ、メチルおよび−ＣＮからなる群から独立して選択される、請求項１〜１１のいずれか一項に記載の化合物。 R 4 represents methyl, R 6 is C 2 -C 6 alkyl substituted with one or more fluoro, R 7 represents hydrogen, R a , R b and R c are hydrogen, fluoro 12. A compound according to any one of claims 1 to 11 independently selected from the group consisting of, chloro, methyl and -CN. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 以下：  Less than:

またはその薬学的に許容される塩もしくは溶媒和物である、請求項１に記載の化合物。Or the compound of Claim 1 which is a pharmaceutically acceptable salt or solvate thereof. 医薬品として使用するための、請求項１〜３１のいずれか一項に記載の化合物。  32. A compound according to any one of claims 1 to 31 for use as a medicament. 哺乳動物におけるＨＢＶ感染の予防または処置に使用される、請求項１〜３１のいずれか一項に記載の化合物。 32. A compound according to any one of claims 1 to 31 for use in the prevention or treatment of HBV infection in a mammal. 請求項１〜３１のいずれか一項に記載の化合物と、薬学的に許容される担体とを含む医薬組成物。 32. A pharmaceutical composition comprising the compound according to any one of claims 1 to 31 and a pharmaceutically acceptable carrier. 哺乳動物におけるＨＢＶ感染を予防または処置するための医薬組成物であって、請求項１〜３１のいずれか一項に記載の化合物を含む、医薬組成物。  A pharmaceutical composition for preventing or treating HBV infection in a mammal, comprising the compound according to any one of claims 1 to 31. ＨＢＶ感染の処置において同時に、別々に、または順次使用される併用剤として、（ａ）請求項１〜３１のいずれか一項に記載の式（ＩＤ）の化合物またはその薬学的に許容される塩もしくは溶媒和物と、（ｂ）別のＨＢＶ阻害剤とを含有する製品。 (A) a compound of formula (ID) according to any one of claims 1 to 31 or a pharmaceutically acceptable salt thereof as a concomitant used simultaneously, separately or sequentially in the treatment of HBV infection Alternatively, a product containing a solvate and (b) another HBV inhibitor. 請求項１〜３１のいずれか一項に記載の化合物を含む医薬組成物であって、別のＨＢＶ阻害剤と併用して使用されるための、医薬組成物。  A pharmaceutical composition comprising the compound according to any one of claims 1 to 31, for use in combination with another HBV inhibitor.
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